WO2021102359A3 - Taspase1 inhibitors and uses thereof - Google Patents

Taspase1 inhibitors and uses thereof Download PDF

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Publication number
WO2021102359A3
WO2021102359A3 PCT/US2020/061657 US2020061657W WO2021102359A3 WO 2021102359 A3 WO2021102359 A3 WO 2021102359A3 US 2020061657 W US2020061657 W US 2020061657W WO 2021102359 A3 WO2021102359 A3 WO 2021102359A3
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WO
WIPO (PCT)
Prior art keywords
taspase1
inhibitors
taspasel
inhibiting
cancer
Prior art date
Application number
PCT/US2020/061657
Other languages
French (fr)
Other versions
WO2021102359A2 (en
Inventor
Michelle R. Arkin
R. Jeffrey Neitz
Adam R. RENSLO
James Hsieh
Shubhankar DUTTA
Clifford Bryant
William J. Moore
Alex G. Waterson
Lidia Sambucetti
Somnath JANA
Ian M. ROMAINE
Alexander P. LAMERS
Yassir Younis ADAM
Claire REPELLIN
Original Assignee
The Regents Of The University Of California
Washington University In St. Louis
Vanderbilt University
Sri International
The United States Of America, As Represented By The Secretary, Department Of Health And Human Services
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by The Regents Of The University Of California, Washington University In St. Louis, Vanderbilt University, Sri International, The United States Of America, As Represented By The Secretary, Department Of Health And Human Services filed Critical The Regents Of The University Of California
Priority to CN202080092864.4A priority Critical patent/CN115697331A/en
Priority to EP20889515.1A priority patent/EP4065112A4/en
Priority to AU2020386081A priority patent/AU2020386081A1/en
Priority to JP2022529821A priority patent/JP2023503926A/en
Priority to CA3162244A priority patent/CA3162244A1/en
Priority to US17/777,971 priority patent/US20230052528A1/en
Publication of WO2021102359A2 publication Critical patent/WO2021102359A2/en
Publication of WO2021102359A3 publication Critical patent/WO2021102359A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/22—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with hetero atoms directly attached to ring nitrogen atoms
    • C07D295/26—Sulfur atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/11—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic unsaturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40—Y being a hydrogen or a carbon atom
    • C07C323/41—Y being a hydrogen or an acyclic carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12N—MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA
    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/14—Hydrolases (3)
    • C12N9/48—Hydrolases (3) acting on peptide bonds (3.4)
    • C12N9/50—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25)
    • C12N9/64—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue
    • C12N9/6421—Proteinases, e.g. Endopeptidases (3.4.21-3.4.25) derived from animal tissue from mammals
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y304/00—Hydrolases acting on peptide bonds, i.e. peptidases (3.4)
    • C12Y304/25—Threonine endopeptidases (3.4.25)

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Wood Science & Technology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biochemistry (AREA)
  • General Engineering & Computer Science (AREA)
  • Biomedical Technology (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Enzymes And Modification Thereof (AREA)

Abstract

Disclosed herein, inter alia, are compounds and methods for inhibiting Taspasel and the treatment of cancer.
PCT/US2020/061657 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof WO2021102359A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CN202080092864.4A CN115697331A (en) 2019-11-22 2020-11-20 TASPASE1 inhibitors and uses thereof
EP20889515.1A EP4065112A4 (en) 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof
AU2020386081A AU2020386081A1 (en) 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof
JP2022529821A JP2023503926A (en) 2019-11-22 2020-11-20 TASPASE1 inhibitors and uses thereof
CA3162244A CA3162244A1 (en) 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof
US17/777,971 US20230052528A1 (en) 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962939258P 2019-11-22 2019-11-22
US62/939,258 2019-11-22

Publications (2)

Publication Number Publication Date
WO2021102359A2 WO2021102359A2 (en) 2021-05-27
WO2021102359A3 true WO2021102359A3 (en) 2021-07-01

Family

ID=75981716

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2020/061657 WO2021102359A2 (en) 2019-11-22 2020-11-20 Taspase1 inhibitors and uses thereof

Country Status (7)

Country Link
US (1) US20230052528A1 (en)
EP (1) EP4065112A4 (en)
JP (1) JP2023503926A (en)
CN (1) CN115697331A (en)
AU (1) AU2020386081A1 (en)
CA (1) CA3162244A1 (en)
WO (1) WO2021102359A2 (en)

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100234363A1 (en) * 2007-09-19 2010-09-16 Institute Of Medicinal Molecular Design, Inc. Heterocyclic derivative having inhibitory activity on type-i 11 data-hydroxysteroid dehydrogenase
US8501811B2 (en) * 2010-06-17 2013-08-06 Washington University TASPASE1 inhibitors and their uses

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6403595B1 (en) * 1998-02-05 2002-06-11 Takeda Chemical Industries, Ltd. Sulfonamide derivatives, processes for producing the same and utilization thereof
GB0224917D0 (en) * 2002-10-25 2002-12-04 Novartis Ag Organic compounds
BRPI0514444A (en) * 2004-08-27 2008-06-10 Infinity Pharmaceuticals Inc cyclopamine analogues and methods of use of these
CA2654784A1 (en) * 2006-06-09 2007-12-13 Icos Corporation Substituted phenylacetic acids as dp-2 antagonists
US9776979B2 (en) * 2013-09-26 2017-10-03 Sanford-Burnham Medical Research Institute EBI2 modulators
EP3116862B1 (en) * 2014-03-10 2019-04-17 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
WO2016049524A1 (en) * 2014-09-25 2016-03-31 Araxes Pharma Llc Inhibitors of kras g12c mutant proteins
CN117903297A (en) * 2016-09-01 2024-04-19 柏林合作研究学会 Chemoselective coupling of sulfhydryl groups with alkenyl or alkynyl phosphoramides
US11071727B2 (en) * 2018-01-26 2021-07-27 Northwestern University Therapeutic targeting of proteolytic cleavage of the mixed lineage leukemia gene product (MLL1) by taspase1 using kinase inhibitors

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100234363A1 (en) * 2007-09-19 2010-09-16 Institute Of Medicinal Molecular Design, Inc. Heterocyclic derivative having inhibitory activity on type-i 11 data-hydroxysteroid dehydrogenase
US8501811B2 (en) * 2010-06-17 2013-08-06 Washington University TASPASE1 inhibitors and their uses

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
YAHAYA ET AL.: "Solution behavior of hydrophobically associating water-soluble block copolymers of acrylamide and N-benzylacrylamide", POLYMER, vol. 42, 2001, pages 3363 - 3372, XP004313877, DOI: 10.1016/S0032-3861(00)00711-4 *

Also Published As

Publication number Publication date
WO2021102359A2 (en) 2021-05-27
CA3162244A1 (en) 2021-05-27
JP2023503926A (en) 2023-02-01
US20230052528A1 (en) 2023-02-16
CN115697331A (en) 2023-02-03
EP4065112A2 (en) 2022-10-05
AU2020386081A1 (en) 2022-06-02
EP4065112A4 (en) 2023-12-27

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